Pyrotinib dimaleate

Catalog No.S8852 Batch:S885203

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Technical Data

Formula

C40H39ClN6O11
Molecular Weight 815.22 CAS No. 1397922-61-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (122.66 mM)
Ethanol 100 mg/mL (122.66 mM)
Water 16 mg/mL warmed with 50ºC water bath (19.62 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Pyrotinib dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.
Targets
EGFR [1]
(Cell-free assay)		 HER2 [1]
(Cell-free assay)
0.013 μM 0.038 μM
In vitro

Pyrotinib (SHR1258), as an EGFR/HER2 dual tyrosine kinase inhibitor, shows excellent in vitro potency, selectivity, and favorable PK profiles.[1]
In vivo

Pyrotinib (SHR1258) displays robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    A431, SK-BR-3, NCI-N87

  • Concentrations

    6-7 concentrations (not specific)

  • Incubation Time

    72 h

  • Method

    Cells are incubated in a carbon dioxide (5%CO2) incubator until they reached 85% confluency, subsequently, cell culture medium is replaced by fresh one with Pyrotinib (SHR1258) added in a series of concentrations (6 to 7 concentrations). The cells are then put back to the incubator and cultured continuously. After 72 hours, the activity of the test compounds for inhibiting the cell proliferation is determined by a sulforhodamine B (SRB) method.
Animal Study:

[1]
  • Animal Models

    6-7-week-old female BALB/Ca-nude mice with BT-474/SK-OV-3 xenografts

  • Dosages

    2.5-20 mg/kg, 100 mg/kg

  • Administration

    IV, IG

Selleck's Pyrotinib dimaleate has been cited by 3 publications

Activity and mechanism of acquired resistance to tarloxotinib in HER2 mutant lung cancer: an in vitro study [ Transl Lung Cancer Res, 2021, 10(8):3659-3670] PubMed: 34584864
UPLC-MS/MS assay for the simultaneous determination of pyrotinib and its oxidative metabolite in rat plasma: Application to a pharmacokinetic study [ Biomed Chromatogr, 2021, e5221] PubMed: 34331710
Clinical implications of plasma ctDNA features and dynamics in gastric cancer treated with HER2-targeted therapies [ Clin Transl Med, 2020, 10(8):e254] PubMed: 33377634

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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